| 7-酰氨基-3-(1,2,3-三唑甲基)头孢菌素衍生物的合成及其抗菌活性 |
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| 引用本文： | 张存瑜,胡树琛,周慧殊,段廷汉.7-酰氨基-3-(1,2,3-三唑甲基)头孢菌素衍生物的合成及其抗菌活性[J].药学学报,1991,26(3):175-182. |
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| 作者姓名： | 张存瑜 胡树琛 周慧殊 段廷汉 |
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| 作者单位： | 中国药科大学半合成抗生素研究室，中国药科大学半合成抗生素研究室，中国药科大学半合成抗生素研究室，中国药科大学半合成抗生素研究室 南京 210009，南京 210009，南京 210009，南京 210009 |
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| 摘 要： | 本文以青霉素G扩环而得的7-苯乙酰氨基-3-甲基-3-头孢烯-4-羧酸(Ⅰ)为原料,合成了12个C3位上有1,2,3-三唑甲基取代的新头孢菌素衍生物(Ⅷ1～12),并经分析确证了各化合物的结构。体外抑菌试验结果表明,其中6个化合物,即Ⅶ2～4,9～11,不仅对革兰氏阳性菌有较高的抑制作用。而且对革兰氏阴性菌也有高度敏感性。
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| 关 键 词： | 口服头孢菌素 7-酰氨基-3-(1 2 3-三唑甲基)头孢菌素 抗菌活性 构效关系 |
| 收稿时间： | 1989-12-20 |
SYNTHESIS AND ANTIMICROBIAL ACTIVITY OF 7-ACYLAMIDO-3-(1,2,3-TRIAZOL-1-YLMETHYL) CEPHALOSPORINS |
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| CY Zhang,SC Hu,HS Zhou and TH Duan.SYNTHESIS AND ANTIMICROBIAL ACTIVITY OF 7-ACYLAMIDO-3-(1,2,3-TRIAZOL-1-YLMETHYL) CEPHALOSPORINS[J].Acta Pharmaceutica Sinica,1991,26(3):175-182. |
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| Authors: | CY Zhang SC Hu HS Zhou and TH Duan |
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| Institution: | Division of Semisynthetic Antibiotics, China Pharmaceutical University, Nanjing. |
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| Abstract: | In order to develop oral cephalosporin exhibiting broad-spectrum activity, a series of cephalosporin derivatives (VIII1-12) bearing 1, 2, 3-triazolymethyl substituents on the C3 position were synthesized. 7-Phenylacetamido-3-methyl-3-cephem-4-carboxylic acid (I) was employed as starting material and converted to VIII by procedures of esterification and oxidation, bromination, azido-substitution, dipolarcycloaddition, deprotection, cleavage, and condensation. Minimum inhibitory concentration (MIC) values in vitro showed that VIII2-4.9-11 had a wide antibacterial spectrum against Gram positive and Gram negative bacteria and possessed high activities. Further biological evaluation and the study of oral absorption for the six compounds will be performed. |
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| Keywords: | Oral cephalosporin 7-Acylamido-3-(1 2 3-triazol-ylmethyl) cephalosporins Antibacterial activity Structure-activity relationship |
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